[go: up one dir, main page]

PH12020500583A1 - 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases - Google Patents

2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases

Info

Publication number
PH12020500583A1
PH12020500583A1 PH12020500583A PH12020500583A PH12020500583A1 PH 12020500583 A1 PH12020500583 A1 PH 12020500583A1 PH 12020500583 A PH12020500583 A PH 12020500583A PH 12020500583 A PH12020500583 A PH 12020500583A PH 12020500583 A1 PH12020500583 A1 PH 12020500583A1
Authority
PH
Philippines
Prior art keywords
derivatives
pyrazolo
pyrimidin
tetrahydro
inflammatory diseases
Prior art date
Application number
PH12020500583A
Other versions
PH12020500583B1 (en
Inventor
Sylvie Froidevaux
Francis Hubler
Mark Murphy
Dorte Renneberg
Simon Stamm
Original Assignee
Idorsia Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of PH12020500583A1 publication Critical patent/PH12020500583A1/en
Publication of PH12020500583B1 publication Critical patent/PH12020500583B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Eye Examination Apparatus (AREA)
  • Oscillators With Electromechanical Resonators (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)

Abstract

The present invention relates to derivatives of formula (I) wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are The present invention discloses derivatives of formula (I), wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are as described in the description, and in particular e.g. 2,4,6,7-tetrahydro-pyrazolo[4,3- d]pyrimidin-5-one derivatives and related compounds, their preparation, pharmaceutically acceptable salts thereof, their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (I), and especially their use as C5a receptor modulators for treating e.g. vasculitis and inflammatory diseases.
PH1/2020/500583A 2018-01-10 2019-01-09 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases PH12020500583B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2018050598 2018-01-10
PCT/EP2019/050372 WO2019137927A1 (en) 2018-01-10 2019-01-09 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases

Publications (2)

Publication Number Publication Date
PH12020500583A1 true PH12020500583A1 (en) 2021-06-14
PH12020500583B1 PH12020500583B1 (en) 2024-02-21

Family

ID=65012016

Family Applications (1)

Application Number Title Priority Date Filing Date
PH1/2020/500583A PH12020500583B1 (en) 2018-01-10 2019-01-09 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases

Country Status (30)

Country Link
US (2) US11608341B2 (en)
EP (1) EP3737684B1 (en)
JP (1) JP7014914B2 (en)
KR (1) KR102574564B1 (en)
CN (1) CN111566109B (en)
AR (1) AR114564A1 (en)
AU (1) AU2019207666B2 (en)
BR (1) BR112020013788A2 (en)
CA (1) CA3086310C (en)
CL (1) CL2020001817A1 (en)
DK (1) DK3737684T3 (en)
EA (1) EA202091641A1 (en)
ES (1) ES2933820T3 (en)
HR (1) HRP20221449T1 (en)
HU (1) HUE060515T2 (en)
IL (1) IL275868B2 (en)
LT (1) LT3737684T (en)
MA (1) MA51558B1 (en)
MX (1) MX2020007443A (en)
MY (1) MY198902A (en)
PH (1) PH12020500583B1 (en)
PL (1) PL3737684T3 (en)
PT (1) PT3737684T (en)
RS (1) RS63806B1 (en)
SG (1) SG11202006490YA (en)
SI (1) SI3737684T1 (en)
TW (2) TWI839788B (en)
UA (1) UA124694C2 (en)
WO (1) WO2019137927A1 (en)
ZA (1) ZA202004910B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS63806B1 (en) * 2018-01-10 2023-01-31 Idorsia Pharmaceuticals Ltd 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases
EP3740476A1 (en) * 2018-01-19 2020-11-25 Idorsia Pharmaceuticals Ltd C5a receptor modulators
CN111683937A (en) * 2018-01-19 2020-09-18 爱杜西亚药品有限公司 C5a receptor modulators
ES2974660T3 (en) * 2019-07-09 2024-07-01 Idorsia Pharmaceuticals Ltd Pharmaceutical composition comprising a tetrahydropyrazolopyrimidinone compound
US11193891B2 (en) * 2019-12-20 2021-12-07 Robert Bosch Gmbh Receptors and spacers for a fluorescence-based lead ion chemosensor

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003218374A1 (en) 2002-03-28 2003-10-13 Neurogen Corporation Substituted tetrahydroisoquinolines as c5a receptor modulators
WO2004033455A2 (en) * 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
US7906528B2 (en) * 2004-10-05 2011-03-15 Novartis International Pharmaceutical Ltd. Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
BR112012033075B1 (en) 2010-06-24 2021-06-01 Chemocentryx, Inc C5A RECEPTOR ANTAGONIST REPLACED PIPERIDINE COMPOUND, PHARMACEUTICAL COMPOSITION, AND, USE OF COMPOUND
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
TWI657090B (en) * 2013-03-01 2019-04-21 英塞特控股公司 USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3Kδ RELATED DISORDERS
CA2923184A1 (en) 2013-09-04 2015-03-12 Bristol-Myers Squibb Company Compounds useful as immunomodulators
PL3363790T3 (en) 2013-09-06 2020-07-27 Aurigene Discovery Technologies Limited 1,2,4-oxadiazole derivatives as immunomodulators
WO2015044900A1 (en) 2013-09-27 2015-04-02 Aurigene Discovery Technologies Limited Therapeutic immunomodulating compounds
UY36298A (en) * 2014-09-16 2016-04-29 Gilead Science Inc SOLID FORMS OF A TOLL TYPE RECEIVER MODULATOR
US9682940B2 (en) 2015-08-25 2017-06-20 Janssen Pharmaceutica Nv Indazole derivatives useful as CB-1 inverse agonists
RS63806B1 (en) * 2018-01-10 2023-01-31 Idorsia Pharmaceuticals Ltd 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases
EP3740476A1 (en) 2018-01-19 2020-11-25 Idorsia Pharmaceuticals Ltd C5a receptor modulators
CN111683937A (en) 2018-01-19 2020-09-18 爱杜西亚药品有限公司 C5a receptor modulators
ES2974660T3 (en) 2019-07-09 2024-07-01 Idorsia Pharmaceuticals Ltd Pharmaceutical composition comprising a tetrahydropyrazolopyrimidinone compound

Also Published As

Publication number Publication date
EP3737684B1 (en) 2022-11-16
ES2933820T3 (en) 2023-02-14
MA51558B1 (en) 2022-12-30
CN111566109B (en) 2023-07-11
HRP20221449T1 (en) 2023-01-20
TWI774905B (en) 2022-08-21
TWI839788B (en) 2024-04-21
BR112020013788A2 (en) 2020-12-01
MX2020007443A (en) 2020-09-14
JP7014914B2 (en) 2022-02-01
PT3737684T (en) 2022-12-20
SG11202006490YA (en) 2020-08-28
KR102574564B1 (en) 2023-09-04
SI3737684T1 (en) 2023-01-31
IL275868B2 (en) 2023-06-01
AU2019207666B2 (en) 2023-12-21
CN111566109A (en) 2020-08-21
WO2019137927A1 (en) 2019-07-18
KR20200106061A (en) 2020-09-10
IL275868A (en) 2020-08-31
HUE060515T2 (en) 2023-03-28
US20200369672A1 (en) 2020-11-26
AR114564A1 (en) 2020-09-23
TW201930307A (en) 2019-08-01
PH12020500583B1 (en) 2024-02-21
JP2021510373A (en) 2021-04-22
MY198902A (en) 2023-10-02
EA202091641A1 (en) 2020-11-17
US11608341B2 (en) 2023-03-21
ZA202004910B (en) 2024-02-28
LT3737684T (en) 2022-12-27
MA51558A (en) 2021-04-14
CL2020001817A1 (en) 2020-12-04
RS63806B1 (en) 2023-01-31
PL3737684T3 (en) 2023-02-27
EP3737684A1 (en) 2020-11-18
AU2019207666A1 (en) 2020-08-27
UA124694C2 (en) 2021-10-27
CA3086310A1 (en) 2019-07-18
TW202244047A (en) 2022-11-16
DK3737684T3 (en) 2022-12-12
CA3086310C (en) 2023-09-19
US20230192708A1 (en) 2023-06-22

Similar Documents

Publication Publication Date Title
PH12020500583A1 (en) 2,4,6,7-tetrahydro-pyrazolo[4,3-d]pyrimidin-5-one derivatives and related compounds as c5a receptor modulators for treating vasculitis and inflammatory diseases
GEP20217242B (en) Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors
PH12019500188A1 (en) Piperidine cxcr7 receptor modulators
PH12014500919A1 (en) (4-phenylimidazol-2-yl) ethylamine derivatives useful as sodium channel modulators
EP4467549A3 (en) Intermediates of n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
WO2012007877A3 (en) N- sulfonylbenzamides as inhibitors of voltage - gated sodium channels
MX375925B (en) IMIDAZO[1,2-A]PYRAZIN-1-YL-BENZAMIDE COMPOUNDS FOR TREATMENT OF SPINAL MUSCULAR ATROPHY.
PH12021552760A1 (en) 3-amino-4h-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of mrgx2
PH12017501699A1 (en) Fused bicyclic heteroaryl derivatives having activity as phd inhibitors
SA522431777B1 (en) Alpha-d-galactopyranoside derivatives
MX2009010165A (en) New imidazo[ 4,5-b]pyridine-7-carboxamides 704.
PH12021552533A1 (en) Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease
PH12015502632A1 (en) Cxcr7 receptor modulators
MX367772B (en) Novel n-(2,3-dihydro-1h-pyrrolo[2,3-b]jpyrid in-5-yl)-4- quinazolinamine and n-(2,3-dihydro-1h-i ndol-5-yl)-4- quinazolinamine derivatives as perk inhibitors.
MX2020013291A (en) Alkoxy-substituted pyridinyl derivatives as lpa1 receptor antagonists and their use in the treatment of fibrosis.
MX2008012093A (en) New therapeutic combinations for the treatment or prevention of psychotic disorders.
PH12021553178A1 (en) Pyridin-3-yl derivatives
PH12020552236A1 (en) Crystal form of compound for inhibiting the activity of cdk4/6 and use thereof
SI1869038T1 (en) SUBSTITUTED 5,6,7,8-TETRAHYDRO-IMIDAZO?á1,2-A?åPYRIDIN-2-YLAMINE COMPOUNDS AND THEIR USE FOR PRODUCING DRUGS
PH12022550859A1 (en) 2-azaspiro[3.4]octane derivatives as m4 agonists
PH12022550860A1 (en) 5-oxa-2-azaspiro[3.4]octane derivatives as m4 agonists
MX2017011423A (en) 7-(morpholin-4-yl)pyrazole[1,5-a]pyrimidine derivatives which are useful for the treatment of immune or inflammatory diseases or cancer.
MX2020014327A (en) Amino-pyrimidonyl derivatives, a process for their preparation and pharmaceutical compositions containing them.
MX2009013240A (en) Hetero bicyclic carboxamide derivatives and their pharmaceutical use and compositions.